Endothelin receptor antagonists

Abstract

Novel indane and indene derivatives are described which are endothelin receptor antagonists.

We claim: 
     
       1. A compound which is: (1RS, 2SR, 3RS)-3-(2-Carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylene-dioxyphenyl)-5-(prop-1-yloxy)-indane-2-carboxylic acid or a pharmaceutically acceptable salt thereof.   
     
     
       2. A compound which is: (+)(1S, 2R, 3S)-3-(2-Carboxymethoxy-4-methoxyphenyl!-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid; or a pharmaceutically acceptable salt thereof.   
     
     
       3. A compound of claim 2 which is: (+)(1S, 2R, 3S)-3-(2-Carboxymethoxy-4-methoxyphenyl!-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid disodium salt.   
     
     
       4. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier. 
     
     
       5. A method of antagonizing endothelin receptors which comprises administering to a subject in need thereof, an effective amount of a compound of claim 1. 
     
     
       6. A pharmaceutical composition comprising a compound of claim 2 and a pharmaceutically acceptable carrier. 
     
     
       7. A method of antagonizing endothelin receptors which comprises administering to a subject in need thereof, an effective amount to antagonize endothelin receptors of a compound of claim 2. 
     
     
       8. A method of treatment of diseases caused by an excess of endothelin comprising administering to a subject in need thereof, an effective amount of an endothelin receptor antagonist of claim 2. 
     
     
       9. A method of treating hypertension, renal failure or cerebrovascular disease which comprises administering to a subject in need thereof, an effective amount of a compound of claim 2. 
     
     
       10. A method for the prophylaxis and treatment of radiocontrast induced renal failure which comprises administering to a subject in need thereof, an effective amount of a compound of claim 2. 
     
     
       11. A method of treatment of congestive heart failure which comprises administering to a subject in need thereof, an effective amount of a compound of claim 2. 
     
     
       12. A method of treatment of migraine which comprises administering to a subject in need thereof, an effective amount of a compound of claim 2. 
     
     
       13. A method of preventing or treating restenosis which comprises administering to a subject in need thereof, an effective amount of a compound of claim 2. 
     
     
       14. A pharmaceutical composition comprising a compound of claim 3 and a pharmaceutically acceptable carrier. 
     
     
       15. A method of antagonizing endothelin receptors which comprises administering to a subject in need thereof, an effective amount of a compound of claim 3.